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Items: 1 to 20 of 100

1.

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.

Boy KM, Guernon JM, Zuev DS, Xu L, Zhang Y, Shi J, Marcin LR, Higgins MA, Wu YJ, Krishnananthan S, Li J, Trehan A, Smith D, Toyn JH, Meredith JE, Burton CR, Kimura SR, Zvyaga T, Zhuo X, Lentz KA, Grace JE, Denton R, Morrison JS, Mathur A, Albright CF, Ahlijanian MK, Olson RE, Thompson LA, Macor JE.

ACS Med Chem Lett. 2019 Feb 17;10(3):312-317. doi: 10.1021/acsmedchemlett.8b00541. eCollection 2019 Mar 14.

2.

Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.

Toyn JH, Boy KM, Raybon J, Meredith JE Jr, Robertson AS, Guss V, Hoque N, Sweeney F, Zhuo X, Clarke W, Snow K, Denton RR, Zuev D, Thompson LA, Morrison J, Grace J, Berisha F, Furlong M, Wang JS, Lentz KA, Padmanabha R, Cook L, Wei C, Drexler DM, Macor JE, Albright CF, Gasior M, Olson RE, Hong Q, Soares HD, AbuTarif M, Ahlijanian MK.

J Pharmacol Exp Ther. 2016 Jul;358(1):125-37. doi: 10.1124/jpet.116.232249. Epub 2016 Apr 20.

3.

Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.

Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF.

Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8.

4.

Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor.

Barten DM, Guss VL, Corsa JA, Loo A, Hansel SB, Zheng M, Munoz B, Srinivasan K, Wang B, Robertson BJ, Polson CT, Wang J, Roberts SB, Hendrick JP, Anderson JJ, Loy JK, Denton R, Verdoorn TA, Smith DW, Felsenstein KM.

J Pharmacol Exp Ther. 2005 Feb;312(2):635-43. Epub 2004 Sep 27.

PMID:
15452193
5.

Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014.

Lanz TA, Wood KM, Richter KE, Nolan CE, Becker SL, Pozdnyakov N, Martin BA, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B.

J Pharmacol Exp Ther. 2010 Jul;334(1):269-77. doi: 10.1124/jpet.110.167379. Epub 2010 Apr 2.

PMID:
20363853
6.

The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers.

Soares HD, Gasior M, Toyn JH, Wang JS, Hong Q, Berisha F, Furlong MT, Raybon J, Lentz KA, Sweeney F, Zheng N, Akinsanya B, Berman RM, Thompson LA, Olson RE, Morrison J, Drexler DM, Macor JE, Albright CF, Ahlijanian MK, AbuTarif M.

J Pharmacol Exp Ther. 2016 Jul;358(1):138-50. doi: 10.1124/jpet.116.232256. Epub 2016 Apr 20.

7.

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.

Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE.

ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10.

8.

Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897.

Anderson JJ, Holtz G, Baskin PP, Turner M, Rowe B, Wang B, Kounnas MZ, Lamb BT, Barten D, Felsenstein K, McDonald I, Srinivasan K, Munoz B, Wagner SL.

Biochem Pharmacol. 2005 Feb 15;69(4):689-98. Epub 2005 Jan 7.

PMID:
15670587
9.

In vitro and in vivo metabolism of a gamma-secretase inhibitor BMS-299897 and generation of active metabolites in milligram quantities with a microbial bioreactor.

Zhang D, Hanson R, Roongta V, Dischino DD, Gao Q, Sloan CP, Polson C, Keavy D, Zheng M, Mitroka J, Yeola S.

Curr Drug Metab. 2006 Dec;7(8):883-96.

PMID:
17168689
10.

A novel Abeta isoform pattern in CSF reflects gamma-secretase inhibition in Alzheimer disease.

Portelius E, Dean RA, Gustavsson MK, Andreasson U, Zetterberg H, Siemers E, Blennow K.

Alzheimers Res Ther. 2010 Mar 29;2(2):7. doi: 10.1186/alzrt30.

11.
12.

Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator.

Peng H, Talreja T, Xin Z, Cuervo JH, Kumaravel G, Humora MJ, Xu L, Rohde E, Gan L, Jung MY, Shackett MN, Chollate S, Dunah AW, Snodgrass-Belt PA, Arnold HM, Taveras AG, Rhodes KJ, Scannevin RH.

ACS Med Chem Lett. 2011 Aug 5;2(10):786-91. doi: 10.1021/ml200175q. eCollection 2011 Oct 13.

13.

Effects of gamma-secretase inhibition on the amyloid beta isoform pattern in a mouse model of Alzheimer's disease.

Portelius E, Zhang B, Gustavsson MK, Brinkmalm G, Westman-Brinkmalm A, Zetterberg H, Lee VM, Trojanowski JQ, Blennow K.

Neurodegener Dis. 2009;6(5-6):258-62. doi: 10.1159/000264639. Epub 2009 Dec 3.

14.

Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS.

J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11.

PMID:
19671883
15.

Characterization of FRM-36143 as a new γ-secretase modulator for the potential treatment of familial Alzheimer's disease.

Blain JF, Bursavich MG, Freeman EA, Hrdlicka LA, Hodgdon HE, Chen T, Costa DE, Harrison BA, Kapadnis S, Murphy DA, Nolan S, Tu Z, Tang C, Burnett DA, Patzke H, Koenig G.

Alzheimers Res Ther. 2016 Aug 30;8:34. doi: 10.1186/s13195-016-0199-5.

16.

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.

Albright CF, Dockens RC, Meredith JE Jr, Olson RE, Slemmon R, Lentz KA, Wang JS, Denton RR, Pilcher G, Rhyne PW, Raybon JJ, Barten DM, Burton C, Toyn JH, Sankaranarayanan S, Polson C, Guss V, White R, Simutis F, Sanderson T, Gillman KW, Starrett JE Jr, Bronson J, Sverdlov O, Huang SP, Castaneda L, Feldman H, Coric V, Zaczek R, Macor JE, Houston J, Berman RM, Tong G.

J Pharmacol Exp Ther. 2013 Mar;344(3):686-95. doi: 10.1124/jpet.112.199356. Epub 2012 Dec 28.

PMID:
23275065
17.

γ-Secretase processing and effects of γ-secretase inhibitors and modulators on long Aβ peptides in cells.

Ran Y, Cruz PE, Ladd TB, Fauq AH, Jung JI, Matthews J, Felsenstein KM, Golde TE.

J Biol Chem. 2014 Feb 7;289(6):3276-87. doi: 10.1074/jbc.M113.512921. Epub 2013 Dec 18.

18.

Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.

Zheng M, Wang J, Lubinski J, Flint OP, Krishna R, Yao M, Pursley JM, Thakur A, Boulton DW, Santone KS, Barten DM, Anderson JJ, Felsenstein KM, Hansel SB.

Xenobiotica. 2009 Jul;39(7):544-55. doi: 10.1080/00498250902928555.

PMID:
19480557
19.

γ-secretase inhibitors and modulators for the treatment of Alzheimer's disease: disappointments and hopes.

Imbimbo BP, Giardina GA.

Curr Top Med Chem. 2011;11(12):1555-70. Review.

PMID:
21510832
20.

Gamma-secretase inhibitors for Alzheimer's disease: balancing efficacy and toxicity.

Barten DM, Meredith JE Jr, Zaczek R, Houston JG, Albright CF.

Drugs R D. 2006;7(2):87-97. Review.

PMID:
16542055

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